JP2008520688A5 - - Google Patents
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- Publication number
- JP2008520688A5 JP2008520688A5 JP2007543221A JP2007543221A JP2008520688A5 JP 2008520688 A5 JP2008520688 A5 JP 2008520688A5 JP 2007543221 A JP2007543221 A JP 2007543221A JP 2007543221 A JP2007543221 A JP 2007543221A JP 2008520688 A5 JP2008520688 A5 JP 2008520688A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- ethoxy
- phenyl
- chromen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910003849 O-Si Inorganic materials 0.000 claims 9
- 229910003872 O—Si Inorganic materials 0.000 claims 9
- 102000015694 estrogen receptors Human genes 0.000 claims 8
- 108010038795 estrogen receptors Proteins 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 206010020718 hyperplasia Diseases 0.000 claims 5
- 210000000481 breast Anatomy 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 210000001519 tissue Anatomy 0.000 claims 4
- 201000009273 Endometriosis Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000001132 Osteoporosis Diseases 0.000 claims 3
- 206010047791 Vulvovaginal dryness Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 201000006828 endometrial hyperplasia Diseases 0.000 claims 3
- PAUMCYOKUFGQRG-LJAQVGFWSA-N (2s)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-3-(2-trimethylsilylethoxymethyl)-2h-chromen-7-ol Chemical compound C1=CC([C@H]2C(COCC[Si](C)(C)C)=C(C3=CC=C(O)C=C3O2)C)=CC=C1OCCN1CCCCC1 PAUMCYOKUFGQRG-LJAQVGFWSA-N 0.000 claims 2
- YKALNUZJEDZKJG-UHFFFAOYSA-N 6-[4-(2-piperidin-1-ylethoxy)phenyl]-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-ol Chemical compound O1C2=CC(O)=CC=C2C(CCCCC2)=C2C1C(C=C1)=CC=C1OCCN1CCCCC1 YKALNUZJEDZKJG-UHFFFAOYSA-N 0.000 claims 2
- 208000014644 Brain disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000033830 Hot Flashes Diseases 0.000 claims 2
- 206010060800 Hot flush Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- 208000029725 Metabolic bone disease Diseases 0.000 claims 2
- 206010049088 Osteopenia Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- -1 carboxy, amino Chemical group 0.000 claims 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 230000003920 cognitive function Effects 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 230000003412 degenerative effect Effects 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 201000010260 leiomyoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 239000000583 progesterone congener Substances 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- PAUMCYOKUFGQRG-GDLZYMKVSA-N (2r)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-3-(2-trimethylsilylethoxymethyl)-2h-chromen-7-ol Chemical compound C1=CC([C@@H]2C(COCC[Si](C)(C)C)=C(C3=CC=C(O)C=C3O2)C)=CC=C1OCCN1CCCCC1 PAUMCYOKUFGQRG-GDLZYMKVSA-N 0.000 claims 1
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims 1
- NMYMDQSWZHPVOQ-UHFFFAOYSA-N 2-[4-[2-(azepan-1-yl)ethoxy]phenyl]-4-(2-hydroxyethyl)-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(CCO)=CC1C(C=C1)=CC=C1OCCN1CCCCCC1 NMYMDQSWZHPVOQ-UHFFFAOYSA-N 0.000 claims 1
- BCAHYKSCCYDNLZ-UHFFFAOYSA-N 3-(hydroxymethyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(C)=C(CO)C1C(C=C1)=CC=C1OCCN1CCCCC1 BCAHYKSCCYDNLZ-UHFFFAOYSA-N 0.000 claims 1
- FANGYSXRPPSHRV-UHFFFAOYSA-N 4-(2-hydroxyethyl)-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(CCO)=CC1C(C=C1)=CC=C1OCCN1CCCCC1 FANGYSXRPPSHRV-UHFFFAOYSA-N 0.000 claims 1
- SXENAAYLHGRIAZ-UHFFFAOYSA-N 4-cyclopentyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(C2CCCC2)=CC1C(C=C1)=CC=C1OCCN1CCCCC1 SXENAAYLHGRIAZ-UHFFFAOYSA-N 0.000 claims 1
- ZAOFBTDRLXTTRR-UHFFFAOYSA-N 4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(C)=CC1C(C=C1)=CC=C1OCCN1CCCCC1 ZAOFBTDRLXTTRR-UHFFFAOYSA-N 0.000 claims 1
- PAUMCYOKUFGQRG-UHFFFAOYSA-N 4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-3-(2-trimethylsilylethoxymethyl)-2h-chromen-7-ol Chemical compound O1C2=CC(O)=CC=C2C(C)=C(COCC[Si](C)(C)C)C1C(C=C1)=CC=C1OCCN1CCCCC1 PAUMCYOKUFGQRG-UHFFFAOYSA-N 0.000 claims 1
- IFANTIOZECIHCH-UHFFFAOYSA-N 5-[4-(2-piperidin-1-ylethoxy)phenyl]-1,2,4,5-tetrahydropyrano[3,4-c]chromen-8-ol Chemical compound O1C2=CC(O)=CC=C2C(CCOC2)=C2C1C(C=C1)=CC=C1OCCN1CCCCC1 IFANTIOZECIHCH-UHFFFAOYSA-N 0.000 claims 1
- QYHKGMAAOCANDP-UHFFFAOYSA-N 6-[4-[2-(dimethylamino)ethoxy]phenyl]-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-ol Chemical compound C1=CC(OCCN(C)C)=CC=C1C1C(CCCCC2)=C2C2=CC=C(O)C=C2O1 QYHKGMAAOCANDP-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002785 azepinyl group Chemical group 0.000 claims 1
- 238000011262 co‐therapy Methods 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- RLJYJQLEYYYFCL-UHFFFAOYSA-N tert-butyl-dimethyl-[[5-[4-(2-piperidin-1-ylethoxy)phenyl]-1,2,4,5-tetrahydropyrano[3,4-c]chromen-8-yl]oxy]silane Chemical compound O1C2=CC(O[Si](C)(C)C(C)(C)C)=CC=C2C(CCOC2)=C2C1C(C=C1)=CC=C1OCCN1CCCCC1 RLJYJQLEYYYFCL-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62898704P | 2004-11-18 | 2004-11-18 | |
| PCT/US2005/041648 WO2006055694A1 (en) | 2004-11-18 | 2005-11-17 | Novel 2h-chromene derivatives as selective estrogen receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008520688A JP2008520688A (ja) | 2008-06-19 |
| JP2008520688A5 true JP2008520688A5 (enExample) | 2009-01-15 |
Family
ID=35883498
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007543221A Withdrawn JP2008520688A (ja) | 2004-11-18 | 2005-11-17 | 選択的エストロゲン受容体モジュレーターとしての新規な２ｈ−クロメン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20060166933A1 (enExample) |
| EP (1) | EP1812417B1 (enExample) |
| JP (1) | JP2008520688A (enExample) |
| CN (1) | CN101103011A (enExample) |
| AT (1) | ATE412643T1 (enExample) |
| AU (1) | AU2005307704A1 (enExample) |
| CA (1) | CA2587669A1 (enExample) |
| DE (1) | DE602005010735D1 (enExample) |
| DK (1) | DK1812417T3 (enExample) |
| ES (1) | ES2314747T3 (enExample) |
| PL (1) | PL1812417T3 (enExample) |
| PT (1) | PT1812417E (enExample) |
| SI (1) | SI1812417T1 (enExample) |
| WO (1) | WO2006055694A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6768711B2 (ja) * | 2015-05-26 | 2020-10-14 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 複素環式エストロゲン受容体モジュレーター及びその使用 |
| WO2020024977A1 (zh) * | 2018-08-01 | 2020-02-06 | 陕西麦科奥特科技有限公司 | 用于治疗神经系统疾病的化合物及其应用 |
| CN119176799B (zh) * | 2024-09-19 | 2025-10-03 | 晨伫(杭州)生物科技有限责任公司 | 色烯衍生物及其应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6060503A (en) * | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| DE10013782A1 (de) * | 2000-03-15 | 2001-10-18 | Schering Ag | 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| DE60220179T2 (de) * | 2001-11-19 | 2008-02-07 | Eli Lilly And Co., Indianapolis | Substituierte benzopyrane als selektive agonisten am östrogenrezeptor-beta |
| US7329654B2 (en) * | 2001-12-19 | 2008-02-12 | Janssen Pharmaceutica N.V. | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
-
2005
- 2005-11-17 US US11/281,074 patent/US20060166933A1/en not_active Abandoned
- 2005-11-17 CA CA002587669A patent/CA2587669A1/en not_active Abandoned
- 2005-11-17 DE DE602005010735T patent/DE602005010735D1/de not_active Expired - Fee Related
- 2005-11-17 PL PL05824228T patent/PL1812417T3/pl unknown
- 2005-11-17 ES ES05824228T patent/ES2314747T3/es not_active Expired - Lifetime
- 2005-11-17 DK DK05824228T patent/DK1812417T3/da active
- 2005-11-17 EP EP05824228A patent/EP1812417B1/en not_active Expired - Lifetime
- 2005-11-17 PT PT05824228T patent/PT1812417E/pt unknown
- 2005-11-17 JP JP2007543221A patent/JP2008520688A/ja not_active Withdrawn
- 2005-11-17 AT AT05824228T patent/ATE412643T1/de not_active IP Right Cessation
- 2005-11-17 SI SI200530558T patent/SI1812417T1/sl unknown
- 2005-11-17 AU AU2005307704A patent/AU2005307704A1/en not_active Abandoned
- 2005-11-17 CN CNA2005800468519A patent/CN101103011A/zh active Pending
- 2005-11-17 WO PCT/US2005/041648 patent/WO2006055694A1/en not_active Ceased
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